Anthelmintic activity of aminoalcohol and diamine derivatives against the gastrointestinal nematode Teladorsagia circumcincta

Valderas-García, Elora; Vega, Jennifer de la; Bardón, María Álvarez; Agüero, Verónica Castilla Gómez de; Escarcena, Ricardo; López-Pérez, Jose Luis; Rojo-Vázquez, F.A.; Feliciano, Arturo San; Olmo, Esther del; Balaña‐Fouce, Rafael; Martínez‐Valladares, María

doi:10.1016/j.vetpar.2021.109496

Cited by 6 publications

(11 citation statements)

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“… Cytotoxicity data were reported in a previous study [ 21 ]. Bn: benzyl; Boc: tert -butoxycarbonyl; Bu: n -butyl; CC 50 : cytotoxic concentration 50; Dec: n -decyl; Et: ethyl; Hex: n -hexyl; IC 50 : inhibitory concentration 50; N: length of the alkylside chain; R: radical; SI: selectivity index.…”

Section: Resultsmentioning

confidence: 99%

“…Based on these assumptions, in the present study, a total of 15 AO and 11 AA derivatives, both structurally related to sphingosine, and 15 benzimidazole derivatives were tested against L 1 of T. muris and adult stages of T. muris and H. polygyrus . The anthelmintic activity of most of these compounds was previously tested in vitro against the gastrointestinal nematode infecting sheep Teladorsagia circumcincta [ 18 , 21 ] and some of them were also tested against Leishmania spp. [ 31 , 32 ], Trypanosoma spp.…”

Section: Discussionmentioning

confidence: 99%

“…Cytotoxicity assays for most compounds were carried out in a previous study on two different cell lines, the human colorectal adenocarcinoma Caco-2 (ATCC ® HTB-37™) and the human hepatocarcinoma HepG2 (ATCC ® HB-8065™), using the Alamar Blue staining method, to estimate their toxicity [ 18 , 21 ]. In the present study, the cytotoxicity of only two compounds, AO14 and AO15, was performed following the protocols mentioned above.…”

Section: Methodsmentioning

confidence: 99%

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Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

et al. 2022

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Background Infections by gastrointestinal nematodes cause significant economic losses and disease in both humans and animals worldwide. The discovery of novel anthelmintic drugs is crucial for maintaining control of these parasitic infections. Methods For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrus in vitro. The compounds tested were derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by > 90% at a single concentration of 100 µM; then, their respective IC50 values were calculated. Those compounds with IC50 < 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10 µM. Results Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values < 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris. Conclusions BZ6 and BZ12 could be considered as a starting point for the synthesis of further structurally related compounds. Graphical Abstract

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

et al. 2022

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“…Based on these assumptions, in the present study, a total of 15 AO and 11 AA derivatives, both structurally related to sphingosine, and 15 benzimidazole derivatives were tested against L 1 of T. muris and adult stages of T. muris and H. polygyrus. The anthelmintic activity of most of these compounds were previously tested in vitro against the gastrointestinal nematode infecting sheep Teladorsagia circumcincta [18,21] and some of them were also tested against Leishmania sp. [31,32], Trypanosoma sp.…”

Section: Discussionmentioning

confidence: 99%

“…Cytotoxicity assays for most compounds were previously carried out in previous study on two different cell lines, the human colorectal adenocarcinoma Caco-2 (ATCC® HTB-37™) and the human hepatocarcinoma HepG2 (ATCC® HB-8065™) using the Alamar Blue staining method, in order to estimate their toxicity [18,21]. In the current study, the cytotoxicity of only two compounds, AO14 and AO15, were performed following the previous protocols mentioned above.…”

Section: Cytotoxicity Assays and Selectivity Indexesmentioning

confidence: 99%

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Valladares

Valderas-García

Häberli

et al. 2022

Preprint

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Background: Infections by gastrointestinal nematodes cause significant economic losses and disease in both human and animals worldwide. The discovery of novel anthelmintic drugs is crucial for maintaining control of these parasitic infections.Methods: For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrus in vitro. The compounds tested were derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by more than 90% at a single concentration of 100 µM, and then, their respective IC50 values were calculated. Those compounds with IC50 lower than 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10µM. Results: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values lower than 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris. Conclusions: BZ6 and BZ12 could be considered as potential candidates for further in vivo efficacy testing.

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Anthelmintic resistance: is a solution possible?

Ahuir-Baraja

Cibot

Llobat

et al. 2021

Experimental Parasitology

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Anthelmintic activity of aminoalcohol and diamine derivatives against the gastrointestinal nematode Teladorsagia circumcincta

Cited by 6 publications

References 51 publications

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Anthelmintic resistance: is a solution possible?

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